专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明申请

US20100210729A1 Methods of inducing terminal differentiation 有权
标题翻译：诱导终末分化的方法
公开(公告)号：US20100210729A1
公开(公告)日：2010-08-19
申请号：US12799368
申请日：2010-04-23
申请人： Victoria M. Richon , Judy H. Chiao , William Kevin Kelly , Thomas A. Miller
发明人： Victoria M. Richon , Judy H. Chiao , William Kevin Kelly , Thomas A. Miller
IPC分类号： A61K31/195 , A61P35/00
CPC分类号： A61K9/4866 , A61K9/0019 , A61K9/1652 , A61K31/13 , A61K31/164 , A61K31/165 , A61K31/19 , A61K31/44 , A61K38/12 , A61K47/12 , A61K47/38
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.
摘要翻译：本发明提供了通过施用包含有效的HDAC抑制剂的药物组合物选择性诱导肿瘤细胞的终末分化，细胞生长停滞和/或细胞凋亡和/或抑制组蛋白脱乙酰酶（HDAC）的方法。本发明的药物组合物中活性化合物的口服生物利用度令人惊奇的高。此外，药物组合物在长时间内意外地引起活性化合物的高，治疗有效的血液水平。本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。

12. 发明申请

US20080119562A1 Methods of Inducing Terminal Differentiation 有权
标题翻译：诱导终点分化的方法
公开(公告)号：US20080119562A1
公开(公告)日：2008-05-22
申请号：US11853700
申请日：2007-09-11
申请人： Victoria M. Richon , Judy H. Chiao , William Kevin Kelly , Thomas A. Miller
发明人： Victoria M. Richon , Judy H. Chiao , William Kevin Kelly , Thomas A. Miller
IPC分类号： A61K31/164 , A61P35/00
CPC分类号： A61K9/4866 , A61K9/0019 , A61K9/1652 , A61K31/13 , A61K31/164 , A61K31/165 , A61K31/19 , A61K31/44 , A61K38/12 , A61K47/12 , A61K47/38
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.
摘要翻译：本发明提供了通过施用包含有效的HDAC抑制剂的药物组合物选择性诱导肿瘤细胞的终末分化，细胞生长停滞和/或细胞凋亡和/或抑制组蛋白脱乙酰酶（HDAC）的方法。本发明的药物组合物中活性化合物的口服生物利用度令人惊奇的高。此外，药物组合物在长时间内意外地引起活性化合物的高，治疗有效的血液水平。本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。

13. 发明授权

US07456219B2 Polymorphs of suberoylanilide hydroxamic acid 有权
公开(公告)号：US07456219B2
公开(公告)日：2008-11-25
申请号：US10600132
申请日：2003-06-19
申请人： Thomas A. Miller , Victoria M. Richon , Judy H. Chiao
发明人： Thomas A. Miller , Victoria M. Richon , Judy H. Chiao
IPC分类号： A61A31/16 , C07C259/04
CPC分类号： A61K31/19 , A61K9/0019 , A61K9/1652 , A61K9/4866 , A61K31/13 , A61K31/165 , A61K31/44 , A61K47/12 , A61K47/38 , C07B2200/13 , C07C259/06
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

14. 发明授权

US07652069B2 Polymorphs of suberoylanilide hydroxamic acid 有权
公开(公告)号：US07652069B2
公开(公告)日：2010-01-26
申请号：US11981367
申请日：2007-10-30
申请人： Thomas A. Miller , Victoria M. Richon
发明人： Thomas A. Miller , Victoria M. Richon
IPC分类号： A61A31/16 , C07C259/04
CPC分类号： A61K31/19 , A61K9/0019 , A61K9/1652 , A61K9/4866 , A61K31/13 , A61K31/165 , A61K31/44 , A61K47/12 , A61K47/38 , C07B2200/13 , C07C259/06
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

15. 发明授权

US07199134B2 Hydroxamic acid compounds and methods of use thereof 失效
公开(公告)号：US07199134B2
公开(公告)日：2007-04-03
申请号：US10817688
申请日：2004-04-01
申请人： Ronald Breslow , Thomas A. Miller , Sandro Belvedere , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
发明人： Ronald Breslow , Thomas A. Miller , Sandro Belvedere , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
IPC分类号： C07D215/38 , C07D215/36 , A61K31/47 , A61K31/44
CPC分类号： C07D211/02 , C07D215/38 , C07D401/12
摘要： The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

16. 发明授权

US08101663B2 Polymorphs of suberoylanilide hydroxamic acid 有权
标题翻译：辛二酰苯胺异羟肟酸的多晶型物
公开(公告)号：US08101663B2
公开(公告)日：2012-01-24
申请号：US12653073
申请日：2009-12-07
申请人： Thomas A. Miller , Victoria M. Richon
发明人： Thomas A. Miller , Victoria M. Richon
IPC分类号： A61K31/165 , C07C259/04
CPC分类号： A61K31/19 , A61K9/0019 , A61K9/1652 , A61K9/4866 , A61K31/13 , A61K31/165 , A61K31/44 , A61K47/12 , A61K47/38 , C07B2200/13 , C07C259/06
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
摘要翻译：本发明提供了通过施用包含有效的HDAC抑制剂的药物组合物选择性诱导肿瘤细胞的终末分化，细胞生长停滞和/或细胞凋亡和/或抑制组蛋白脱乙酰酶（HDAC）的方法。本发明的药物组合物中活性化合物的口服生物利用度令人惊奇的高。此外，药物组合物在长时间内意外地引起活性化合物的高，治疗有效的血液水平。本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。本发明还提供了SAHA的新型I型多晶型物，其特征在于独特的X射线衍射图和差示扫描量热法谱，以及独特的晶体结构。

17. 发明授权

US07799803B2 Hydroxamic acid compounds and methods of use thereof 失效
标题翻译：羟肟酸化合物及其使用方法
公开(公告)号：US07799803B2
公开(公告)日：2010-09-21
申请号：US11710036
申请日：2007-02-22
申请人： Ronald Breslow , Thomas A. Miller , Sandro Belvedere , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
发明人： Ronald Breslow , Thomas A. Miller , Sandro Belvedere , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D211/02 , C07D215/38 , C07D401/12
摘要： The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
摘要翻译：本发明涉及一类具有至少两个含芳基基团的异羟肟酸衍生物，其中至少一个是喹啉基，异喹啉基或苄基部分，通过亚甲基链与异羟肟酸基团连接。异羟肟酸化合物可用于治疗癌症，例如脑癌。异羟肟酸化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经变性疾病

18. 发明申请

US20090042992A1 Polymorphs of suberoylanilide hydroxamic acid 有权
标题翻译：辛二酰苯胺异羟肟酸的多晶型物
公开(公告)号：US20090042992A1
公开(公告)日：2009-02-12
申请号：US12077396
申请日：2008-03-18
申请人： Thomas A. Miller , Victoria M. Richon
发明人： Thomas A. Miller , Victoria M. Richon
IPC分类号： A61K31/164 , A61P35/00
CPC分类号： A61K31/19 , A61K9/0019 , A61K9/1652 , A61K9/4866 , A61K31/13 , A61K31/165 , A61K31/44 , A61K47/12 , A61K47/38 , C07B2200/13 , C07C259/06
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
摘要翻译：本发明提供了通过施用包含有效的HDAC抑制剂的药物组合物选择性诱导肿瘤细胞的终末分化，细胞生长停滞和/或细胞凋亡和/或抑制组蛋白脱乙酰酶（HDAC）的方法。本发明的药物组合物中活性化合物的口服生物利用度令人惊奇的高。此外，药物组合物在长时间内意外地引起活性化合物的高，治疗有效的血液水平。本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。本发明还提供了SAHA的新型I型多晶型物，其特征在于独特的X射线衍射图和差示扫描量热法谱，以及独特的晶体结构。

19. 发明申请

US20080194692A1 Polymorphs of suberoylanilide hydroxamic acid 有权
公开(公告)号：US20080194692A1
公开(公告)日：2008-08-14
申请号：US11981367
申请日：2007-10-30
申请人： Thomas A. Miller , Victoria M. Richon
发明人： Thomas A. Miller , Victoria M. Richon
IPC分类号： A61K31/16 , A61P35/00
CPC分类号： A61K31/19 , A61K9/0019 , A61K9/1652 , A61K9/4866 , A61K31/13 , A61K31/165 , A61K31/44 , A61K47/12 , A61K47/38 , C07B2200/13 , C07C259/06
摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

20. 发明授权

US07126001B2 Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof 有权
标题翻译：细胞分化剂和组蛋白脱乙酰酶抑制剂的类别及其使用方法
公开(公告)号：US07126001B2
公开(公告)日：2006-10-24
申请号：US10281875
申请日：2002-10-25
申请人： Ronald Breslow , Sandro Belvedere , Leland Gershell , Thomas A. Miller , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
发明人： Ronald Breslow , Sandro Belvedere , Leland Gershell , Thomas A. Miller , Paul A. Marks , Victoria M. Richon , Richard A. Rifkind
IPC分类号： C07D215/38 , C07D473/02 , C07C259/04 , A61K31/47
CPC分类号： C07D213/75 , C07C233/07 , C07C233/13 , C07C235/74 , C07C237/12 , C07C237/22 , C07C259/06 , C07C271/22 , C07C311/03 , C07C311/06 , C07C311/42 , C07C327/32 , C07C2601/14 , C07D213/82 , C07D215/38 , C07D215/40 , C07D215/54 , C07D231/12 , C07D231/40 , C07D233/56 , C07D233/64 , C07D249/08 , C07D277/46 , C07D333/38 , C07F9/2458 , C07F9/4465
摘要： The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
摘要翻译：本发明提供具有下式的化合物：其中R 1和R 2各自为取代或未取代的芳基，环烷基，环烷基氨基，石脑油，吡啶氨基，哌啶子基，叔丁基，芳氧基，芳基烷氧基或吡啶基; 其中A是酰氨基部分，-O - ， - S - ， - NH-或-CH 2 - 。并且其中n为3至8的整数。本发明还提供了选择性诱导肿瘤细胞的生长停滞，末端分化和/或凋亡并从而抑制这些细胞增殖的方法。此外，本发明提供了治疗具有以肿瘤细胞增殖为特征的肿瘤的患者的方法。最后，本发明提供包含药学上可接受的载体和治疗上可接受量的上述化合物的药物组合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式